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Potential use of 2-hydroxypropyl-beta-cyclodextrin for preparation of orally disintegrating tablets containing dl-alpha-tocopheryl acetate, an oily drug.

Authors
  • Motoyama, Keiichi
  • Nagatomo, Kiyoshi
  • Abd Elazim, Soliman Osama
  • Hirayama, Fumitoshi
  • Uekama, Kaneto
  • Arima, Hidetoshi
Type
Published Article
Journal
Chemical and Pharmaceutical Bulletin
Publisher
Pharmaceutical Society of Japan
Publication Date
Nov 01, 2009
Volume
57
Issue
11
Pages
1206–1212
Identifiers
PMID: 19881268
Source
Medline
License
Unknown

Abstract

To expand the application of a drug in orally disintegrating tablets, the potential use of beta-cyclodextrin (beta-CyD) and 2-hydroxypropyl-beta-cyclodextrin (HP-beta-CyD) as excipients for the tablets containing dl-alpha-tocopheryl acetate (VE), an oily drug, was evaluated. HP-beta-CyD, not beta-CyD, solubilized VE in water through the formation of higher order of complexes at the molar ratio of 1 : 2 (VE : HP-beta-CyD). When prepared under the optimal preparation conditions, the VE tablets containing lactose and 5% (w/w) of HP-beta-CyD, not beta-CyD, had high hardness more than 4 kg and rapid disintegration within 100 s both in vitro and in vivo. In addition, VE tablets containing lactose and 5% (w/w) of HP-beta-CyD, not beta-CyD, maintained the high hardness and rapid disintegration under the accelerated stability test using different conditions for 4 weeks. Therefore, these results suggest the potential use of HP-beta-CyD, not beta-CyD, as an excipient for orally disintegrating tablets containing VE, an oily drug, in the molding method.

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